New 3,9-ethano-2,3,3a,4,9,9a-hexahydro-1H-benzo (f) isoindole derivatives, are farnesyl transferase inhibitors useful for treating hyperproliferative disorders, e.g. psoriasis, restenosis or especially cancer

摘要

(3aRS, 4SR, 9SR, 9aRS)-9-(Dihalophenyl or benzothienyl)-4,9-ethano-(2-(2-(2-methoxyphenyl)-propenoyl)-2,3,3a,4,9 ,9a-hexahydro-1H-benzo(f)isoindole-3a-carboxylic acids (I) are new. Also new are intermediate isoindoline derivatives (IX). Ethano-hexahydro-benzoisoindole derivatives of formula (I), in racemic or optical isomer form, and their salts are new. Ar = 2,4-, 3,5-, 2,5- or 2,3-dihalophenyl (where the halo atoms are F, Cl or Br); or benzo(b)thienyl; and R = H or 1-4C alkyl. Independent claims are also included for: (1) preparation of (I); (2) new isoindole derivative intermediates of formula (IX), in racemic or optical isomer form; and (3) methods for preparing (IX) and further intermediates of formulae (III; G = G'), (IV) and (V). G' = benzyl; R' = alkyl; and R'' = 1-3C alkyl.